Pyrone scaffolds are often present in natural products and many derivatives therefore exhibit favorable biocompatibility and toxicity profiles. Hydroxypyrones are obtained from natural sources or can be synthesized by different well established approaches and may easily be converted into the analogous thiopyrones and hydroxypyridones. These features make them well suited to drug development and other biological applications. Herein, we summarize recent literature on the use of (thio)pyr(id)ones in bioinorganic chemistry with a focus on their metal ion chelating properties. Selected examples and different approaches using (thio)pyr(id)ones are presented and the influence of structural modifications on their chemical, physical and biological properties are discussed. Recent literature on the use of (thio)pyr(id)ones in bioinorganic chemistry is summarized, highlighting in particular their ion metal chelating properties. Selected examples and different approaches using (thio)pyr(id)ones are presented and the influence of structural modifications on the chemical, physical and biological properties are discussed. Display omitted ► (Thio)pyr(id)onato ligands and their metal complexes. ► Application in medicinal inorganic chemistry. ► Tunable ligand system with regard to metal complex stability. ► Potent anticancer active compounds.